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AU671797B2 - Optically active 5H-pyrrolo(3,4-b)pyrazine derivative, its preparation and pharmaceutical compositions containing same - Google Patents

Optically active 5H-pyrrolo(3,4-b)pyrazine derivative, its preparation and pharmaceutical compositions containing same Download PDF

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Publication number
AU671797B2
AU671797B2 AU12264/92A AU1226492A AU671797B2 AU 671797 B2 AU671797 B2 AU 671797B2 AU 12264/92 A AU12264/92 A AU 12264/92A AU 1226492 A AU1226492 A AU 1226492A AU 671797 B2 AU671797 B2 AU 671797B2
Authority
AU
Australia
Prior art keywords
dextrorotatory
isomer
pyrrolo
salt
optically active
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired
Application number
AU12264/92A
Other languages
English (en)
Other versions
AU1226492A (en
Inventor
Claude Cotrel
Gerard Roussel
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Sunovion Pharmaceuticals Inc
Original Assignee
Rhone Poulenc Rorer SA
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=9408772&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AU671797(B2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Rhone Poulenc Rorer SA filed Critical Rhone Poulenc Rorer SA
Publication of AU1226492A publication Critical patent/AU1226492A/en
Application granted granted Critical
Publication of AU671797B2 publication Critical patent/AU671797B2/en
Assigned to AVENTIS PHARMA S.A. reassignment AVENTIS PHARMA S.A. Request to Amend Deed and Register Assignors: RHONE-POULENC RORER S.A.
Assigned to SEPRACOR INC. reassignment SEPRACOR INC. Alteration of Name(s) in Register under S187 Assignors: AVENTIS PHARMA S.A.
Anticipated expiration legal-status Critical
Expired legal-status Critical Current

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pain & Pain Management (AREA)
  • Anesthesiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
AU12264/92A 1991-01-17 1992-01-16 Optically active 5H-pyrrolo(3,4-b)pyrazine derivative, its preparation and pharmaceutical compositions containing same Expired AU671797B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
FR9100490A FR2671800B1 (fr) 1991-01-17 1991-01-17 Derive de la 5h-pyrrolo[3,4-b]pyrazine optiquement actif, sa preparation et les compositions pharmaceutiques qui le contiennent.
FR9100490 1991-01-17
PCT/FR1992/000031 WO1992012980A1 (fr) 1991-01-17 1992-01-16 DERIVE DE LA 5H-PYRROLO[3,4-b]PYRAZINE OPTIQUEMENT ACTIF, SA PREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LE CONTIENNENT

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU30321/95A Division AU3032195A (en) 1991-01-17 1995-08-30 Optically active 5H-pyrrolo(3,4-b)pyrazine derivative, its preparation and pharmaceutical compositions containing it

Publications (2)

Publication Number Publication Date
AU1226492A AU1226492A (en) 1992-08-27
AU671797B2 true AU671797B2 (en) 1996-09-12

Family

ID=9408772

Family Applications (2)

Application Number Title Priority Date Filing Date
AU12264/92A Expired AU671797B2 (en) 1991-01-17 1992-01-16 Optically active 5H-pyrrolo(3,4-b)pyrazine derivative, its preparation and pharmaceutical compositions containing same
AU30321/95A Abandoned AU3032195A (en) 1991-01-17 1995-08-30 Optically active 5H-pyrrolo(3,4-b)pyrazine derivative, its preparation and pharmaceutical compositions containing it

Family Applications After (1)

Application Number Title Priority Date Filing Date
AU30321/95A Abandoned AU3032195A (en) 1991-01-17 1995-08-30 Optically active 5H-pyrrolo(3,4-b)pyrazine derivative, its preparation and pharmaceutical compositions containing it

Country Status (29)

Country Link
US (5) US6319926B1 (he)
EP (2) EP0495717A1 (he)
JP (1) JPH06504548A (he)
AR (1) AR248024A1 (he)
AT (1) ATE121089T1 (he)
AU (2) AU671797B2 (he)
CA (1) CA2099782C (he)
CZ (1) CZ281011B6 (he)
DE (1) DE69202060T2 (he)
DK (1) DK0609210T3 (he)
ES (1) ES2071486T3 (he)
FI (1) FI100331B (he)
FR (1) FR2671800B1 (he)
HU (1) HU218928B (he)
IE (1) IE66110B1 (he)
IL (1) IL100677A (he)
MA (1) MA22392A1 (he)
MX (1) MX9200180A (he)
NO (1) NO179911C (he)
NZ (1) NZ241313A (he)
OA (1) OA09807A (he)
PH (1) PH30982A (he)
PL (1) PL166976B1 (he)
RU (1) RU2110519C1 (he)
SK (1) SK279060B6 (he)
TN (1) TNSN92004A1 (he)
WO (1) WO1992012980A1 (he)
YU (1) YU48878B (he)
ZA (1) ZA92302B (he)

Families Citing this family (50)

* Cited by examiner, † Cited by third party
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FR2671800B1 (fr) 1991-01-17 1993-03-12 Rhone Poulenc Rorer Sa Derive de la 5h-pyrrolo[3,4-b]pyrazine optiquement actif, sa preparation et les compositions pharmaceutiques qui le contiennent.
US5786357A (en) * 1991-12-02 1998-07-28 Sepracor Inc. Methods and compositions for treating sleep disorders, convulsive seizures and other disorders using optically pure (+) zopiclone
ES2101653B1 (es) * 1995-07-10 1998-04-01 Asturpharma S A (+)-6-(5-cloropirid-2-il)-7-oxo-viniloxicarboniloxi-5,6-dihidropirrolo(3,4b)pirazina y su uso para un procedimiento de preparacion de (+)-6-(5-cloropirid-2-il)-5-(4-metilpiperazin-1-il)-carboniloxi-7-oxo-5,6-dihidropirrolo(3,4b)pirazina.
US6339086B1 (en) * 1999-05-14 2002-01-15 Swpracor, Inc. Methods of making and using N-desmethylzopiclone
TW200734460A (en) 1999-10-04 2007-09-16 Ajinomoto Kk Genes for heat resistant enzymes of amino acid biosynthetic pathway derived from thermophilic coryneform bacteria
PL1691811T3 (pl) * 2003-12-11 2014-12-31 Sunovion Pharmaceuticals Inc Skojarzenie leku uspokajającego i modulatora neuroprzekaźnikowego oraz sposoby poprawy jakości snu i leczenia depresji
WO2005063248A1 (en) * 2003-12-22 2005-07-14 Sepracor Inc. Modafinil combination therapy for improving sleep quality
CA2551637A1 (en) * 2003-12-24 2005-07-14 Sepracor Inc. Melatonin combination therapy for improving sleep quality
EP1742624B1 (en) * 2004-02-18 2010-01-06 Sepracor, Inc. Dopamine-agonist combination therapy with sedatives for improving sleep quality
US7776858B2 (en) * 2004-04-05 2010-08-17 Sepracor Inc. Methods of treatment of chronic pain using eszopiclone
EP1919912A1 (en) * 2005-06-21 2008-05-14 Merck Generics (UK) Limited Process for enantiomeric separation of zopiclone
CN101553217A (zh) * 2005-07-06 2009-10-07 塞普拉科公司 艾司佐匹克隆与反式4-(3,4-二氯苯基)-1,2,3,4-四氢-n-甲基-1-萘胺或反式4-(3,4-二氯苯基)-1,2,3,4-四氢-1-萘胺的组合以及治疗绝经期和心境障碍、焦虑症和认知障碍的方法
AU2006265008A1 (en) * 2005-07-06 2007-01-11 Sepracor Inc. Combinations of eszopiclone and O-desmethylvenlafaxine, and methods of treatment of menopause and mood, anxiety, and cognitive disorders
US7476737B2 (en) * 2005-09-05 2009-01-13 Dr. Reddy's Laboratories Limited Eszopiclone process
US20070098788A1 (en) * 2005-10-28 2007-05-03 Gore Subhash P Non-benzodiazepine hypnotic compositions
AU2006308889A1 (en) 2005-10-31 2007-05-10 Braincells, Inc. GABA receptor mediated modulation of neurogenesis
US7863273B2 (en) * 2006-01-17 2011-01-04 Glenmark Generics Ltd. Process for the preparation of an optically active 5H-pyrrolo [3,4-B] pyrazine derivative
US20070203145A1 (en) * 2006-02-03 2007-08-30 Jie Zhu Zopiclone resolution
US20080027223A1 (en) * 2006-03-23 2008-01-31 Teva Pharmaceutical Industries Ltd. Polymorphs of eszopiclone malate
US20070270590A1 (en) * 2006-04-20 2007-11-22 Marioara Mendelovici Methods for preparing eszopiclone crystalline form a, substantially pure eszopiclone and optically enriched eszopiclone
EP1904499A1 (en) * 2006-06-26 2008-04-02 Teva Pharmaceutical Industries Ltd Process for the preparation of zopiclone
US7786304B2 (en) * 2006-11-06 2010-08-31 Centaur Pharmaceutical Pvt. Ltd. Process for the preparation of eszopiclone
TW200846340A (en) * 2007-01-31 2008-12-01 Teva Pharma Methods for preparing eszopiclone
ATE515259T1 (de) * 2007-05-29 2011-07-15 Lek Pharmaceuticals Pharmazeutische zusammensetzung mit eszopiclon
US20080305171A1 (en) * 2007-06-07 2008-12-11 Kristin Anne Arnold Pyrrolopyrazine, formulations, methods of manufacture, and methods of use there
US20090018336A1 (en) * 2007-06-25 2009-01-15 Nina Finkelstein Racemization process of R-zopiclone
EP2020403A1 (en) 2007-08-02 2009-02-04 Esteve Quimica, S.A. Process for the resolution of zopiclone and intermediate compounds
WO2009063486A2 (en) * 2007-08-06 2009-05-22 Usv Limited Process for preparation of dextrorotatory isomer of 6-(5-chloro-pyrid-2-yi)-5-[(4-methyl -1-piperazinyl) carbonyloxy]-7-oxo-6,7-dihydro-5h-pyrrolo [3,4-b] pyrazine (eszopiclone)
CA2747000C (en) * 2007-12-19 2013-09-03 Sunovion Pharmaceuticals Inc. Maleate, besylate, and l-malate salts of 6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5h-pyrrolo[3,4-b]pyrazine
US8269005B2 (en) * 2007-12-19 2012-09-18 Sunovion Pharmaceuticals Inc. L-malate salts of 6-(5-chloro-2-Pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-Oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine
US8198278B2 (en) 2007-12-19 2012-06-12 Sunovion Pharmaceuticals Inc. Besylate salts of 6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine
WO2009085988A1 (en) * 2007-12-19 2009-07-09 Sepracor Inc. Salts of 6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7- dihydro-5h-pyrrolo[3,4-b]pyrazine
US8212036B2 (en) 2007-12-19 2012-07-03 Sunovion Pharmaceuticals Inc. Maleate salts of 6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine
US8268832B2 (en) * 2007-12-19 2012-09-18 Sunovion Pharmaceuticals Inc. Maleate salts of 6-(5-chloro-2-Pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine
US8198277B2 (en) * 2007-12-19 2012-06-12 Sunovion Pharmaceuticals Inc. L-malate salts of 6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine
WO2009101634A2 (en) * 2008-02-13 2009-08-20 Lupin Limited A novel process for the preparation of eszopiclone
AU2009223153A1 (en) 2008-03-12 2009-09-17 Emory University Use of GABAa receptor antagonists for the treatment of excessive sleepiness and disorders associated with excessive sleepiness
US20090269409A1 (en) * 2008-04-24 2009-10-29 Mukesh Kumar Garg Pharmaceutical compositions comprising eszopiclone
CN101607961B (zh) * 2008-06-18 2011-08-10 天津天士力集团有限公司 一种右佐匹克隆结晶及其组合物
JP2012508219A (ja) 2008-11-07 2012-04-05 シプラ・リミテッド ゾピクロンを分割するための方法
EP2370136A4 (en) * 2008-12-01 2015-12-30 Map Pharmaceuticals Inc INHALATIVE RELEASE PROCEDURES AND DEVICES
WO2010074753A1 (en) * 2008-12-23 2010-07-01 Map Pharmaceuticals, Inc. Inhalation devices and related methods for administration of sedative hypnotic compounds
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WO2010116385A2 (en) 2009-04-08 2010-10-14 Rubicon Research Private Limited Pharmaceutical compositions for alleviating unpleasant taste
EP2345654A1 (en) 2010-01-05 2011-07-20 LEK Pharmaceuticals d.d. Eszopiclone particles and a process for their preparation
EP2345655A1 (en) 2010-01-05 2011-07-20 LEK Pharmaceuticals d.d. A process for racemisation of 6-(5-chloropyridin-2-yl)-7-(4-methyl-1-piperazinyl)carbonyloxy-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine
CN103193779B (zh) * 2012-01-05 2016-04-20 成都弘达药业有限公司 一种右佐匹克隆的制备方法
CA3053189A1 (en) * 2012-12-20 2014-06-26 Kashiv Biosciences, Llc Orally disintegrating tablet formulation for enhanced bioavailability
US9636340B2 (en) 2013-11-12 2017-05-02 Ayyappan K. Rajasekaran Kinase inhibitors
JP2020007252A (ja) * 2018-07-05 2020-01-16 アクティブファーマ株式会社 エスゾピクロンジベンゾイル−d−酒石酸塩の製造方法、エスゾピクロンの製造方法、及びエスゾピクロンジベンゾイル−d−酒石酸塩の結晶

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3862149A (en) * 1972-01-07 1975-01-21 Rhone Poulenc Sa Pyrrolo (3,4-b) pyrazine derivatives
US4220646A (en) * 1974-11-07 1980-09-02 Rhone-Poulenc Industries Heterocyclic compounds

Family Cites Families (10)

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US4868214A (en) 1987-11-17 1989-09-19 Analgesic Associates Onset-hastened/enhanced analgesia
US4962124A (en) 1987-11-17 1990-10-09 Analgesic Associates Onset-hastened/enhanced antipyretic response
US5102890A (en) 1989-09-05 1992-04-07 Rhone-Poulenc Sante Pyrrole derivatives, their preparation and pharmaceutical compositions which contain them
FR2671800B1 (fr) * 1991-01-17 1993-03-12 Rhone Poulenc Rorer Sa Derive de la 5h-pyrrolo[3,4-b]pyrazine optiquement actif, sa preparation et les compositions pharmaceutiques qui le contiennent.
WO1993010788A1 (en) 1991-12-02 1993-06-10 Sepracor, Inc. Methods and compositions for treating sleep disorders, convulsive seizures, and other disorders using optically pure (-) zopiclone
US5786357A (en) 1991-12-02 1998-07-28 Sepracor Inc. Methods and compositions for treating sleep disorders, convulsive seizures and other disorders using optically pure (+) zopiclone
US5331000A (en) 1992-03-09 1994-07-19 Sepracor Inc. Antipyretic and analgesic methods and compositions containing optically pure R(-) ketoprofen
US6436926B1 (en) * 1999-05-10 2002-08-20 Medpointe, Inc. Compositions and methods for treating superficial fungal infections
US7476737B2 (en) * 2005-09-05 2009-01-13 Dr. Reddy's Laboratories Limited Eszopiclone process
US20070203145A1 (en) * 2006-02-03 2007-08-30 Jie Zhu Zopiclone resolution

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3862149A (en) * 1972-01-07 1975-01-21 Rhone Poulenc Sa Pyrrolo (3,4-b) pyrazine derivatives
US4220646A (en) * 1974-11-07 1980-09-02 Rhone-Poulenc Industries Heterocyclic compounds

Also Published As

Publication number Publication date
ZA92302B (en) 1992-10-28
PL166976B1 (pl) 1995-07-31
US20050043311A1 (en) 2005-02-24
ES2071486T3 (es) 1995-06-16
OA09807A (fr) 1994-04-15
WO1992012980A1 (fr) 1992-08-06
SK279060B6 (sk) 1998-06-03
US6864257B2 (en) 2005-03-08
US20020193378A1 (en) 2002-12-19
CZ138093A3 (en) 1994-02-16
IL100677A0 (en) 1992-09-06
US6444673B1 (en) 2002-09-03
HUT68915A (en) 1995-08-28
CZ281011B6 (cs) 1996-05-15
ATE121089T1 (de) 1995-04-15
EP0609210B1 (fr) 1995-04-12
NO931919L (no) 1993-05-26
RU2110519C1 (ru) 1998-05-10
JPH06504548A (ja) 1994-05-26
NO179911B (no) 1996-09-30
DK0609210T3 (da) 1995-07-03
IE66110B1 (en) 1995-12-13
MA22392A1 (fr) 1992-10-01
HU9302063D0 (en) 1993-10-28
MX9200180A (es) 1992-07-01
NZ241313A (en) 1993-03-26
AU3032195A (en) 1995-11-09
PH30982A (en) 1997-12-23
US6319926B1 (en) 2001-11-20
US20060194806A1 (en) 2006-08-31
AR248024A1 (es) 1995-05-31
FI933248A0 (fi) 1993-07-16
DE69202060T2 (de) 1995-10-26
FR2671800B1 (fr) 1993-03-12
DE69202060D1 (de) 1995-05-18
SK71993A3 (en) 1993-12-08
EP0609210A4 (fr) 1993-09-17
FI933248L (fi) 1993-07-16
TNSN92004A1 (fr) 1993-06-08
HU218928B (hu) 2000-12-28
NO179911C (no) 1997-01-08
IL100677A (he) 1995-11-27
US7125874B2 (en) 2006-10-24
FI100331B (fi) 1997-11-14
IE920126A1 (en) 1992-07-29
YU5592A (sh) 1994-11-15
AU1226492A (en) 1992-08-27
US7381724B2 (en) 2008-06-03
EP0495717A1 (fr) 1992-07-22
FR2671800A1 (fr) 1992-07-24
CA2099782A1 (fr) 1992-07-18
NO931919D0 (no) 1993-05-26
YU48878B (sh) 2002-09-19
EP0609210A1 (fr) 1994-08-10
CA2099782C (fr) 2002-12-03

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Legal Events

Date Code Title Description
HB Alteration of name in register

Owner name: AVENTIS PHARMA S.A.

Free format text: FORMER NAME WAS: RHONE-POULENC RORER S.A.